57777-33-0Relevant academic research and scientific papers
HETEROCYCLIC GLP-1 AGONISTS
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Paragraph 240, (2022/02/15)
This disclosure relates to GLP-1 agonists of Formula (I), including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.
SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF
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Page/Page column 400; 401, (2014/09/29)
Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
Synthesis and biological evaluation of N-heterocyclic indolyl glyoxylamides as orally active anticancer agents
Li, Wen-Tai,Hwang, Der-Ren,Chen, Ching-Ping,Shen, Chien-Wei,Huang, Chen-Long,Chen, Tung-Wei,Lin, Chi-Hung,Chang, Yee-Ling,Chang, Ying-Ying,Lo, Yue-Kan,Tseng, Huan-Yi,Lin, Chu-Chung,Song, Jeng-Shin,Chen, Hua-Chien,Chen, Shu-Jen,Wu, Se-Hui,Chen, Chiung-Tong
, p. 1706 - 1715 (2007/10/03)
A series of N-heterocyclic indolyl glyoxylamides were synthesized and evaluated for in vitro and in vivo anticancer activities. They exhibited a broad spectrum of anticancer activity not only in murine leukemic cancer cells but also in human gastric, breast, and uterus cancer cells as well as their multidrug resistant sublines with a wide range of IC50 values. They also induced apoptosis and caused DNA fragmentation in human gastric cancer cells. Among the compounds studied, 7 showed the most potent activity of growth inhibition (IC50 17-1711 nM) in several human cancer cells. Given orally, compounds 7 and 13 dose-dependently prolonged the survival of animals inoculated with P388 leukemic cancer cells. N-Heterocyclic indolyl glyoxylamides may be useful as orally active chemotherapeutic agents against cancer and refractory cancerous diseases of multidrug resistance phenotype.
Regioisomeric 3-, 4- and 5-aminomethyl isoxazoles: Synthesis and muscarinic activity
Dannhardt,Kiefer,Lambrecht,Laufer,Mutschler,Schweiger,Striegel
, p. 839 - 850 (2007/10/03)
A series of 3-, 4- and 5-aminomethyl isoxazoles and isoxazoles with one or two additional methyl groups at the heterocycle were synthesized in order to investigate the structural requirements, ie heterocyclic moiety, regiochemistry and length of an aminoalkyl unit, for muscarinic activity. This was assayed on isolated rabbit vas deferens (M1 receptor subtype) and isolated guinea-pig atrium (M2 receptor subtype) and ileum (M3 receptor subtype). The isoxazoles tested are one to three orders of magnitude less active than furane or oxadiazole derivatives, having similar structural characteristics except for the heterocycle. Thus, the differences in molecular point charges and charge distribution contribute to the muscarinic activity of these compounds more than small differences in molecular shape and conformational energies.
